Assay Detail
Binding
CHEMBL4721180
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST tagged EGFR (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.49 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.30 |
| CHEMBL4789811 | — | — | 1 | 8.89 |
| CHEMBL4792426 | — | — | 1 | 8.59 |
| CHEMBL4790655 | — | — | 1 | 8.52 |
| CHEMBL4752951 | — | — | 1 | 8.37 |
| CHEMBL4750196 | — | — | 1 | 8.30 |
| CHEMBL4777353 | — | — | 1 | 8.20 |
| CHEMBL4757724 | — | — | 1 | 8.18 |
| CHEMBL4782025 | — | — | 1 | 8.08 |
| CHEMBL4745521 | — | — | 1 | 8.04 |
| CHEMBL4754811 | — | — | 1 | 7.89 |
| CHEMBL4753193 | — | — | 1 | 7.89 |
| CHEMBL4743566 | — | — | 1 | 7.85 |
| CHEMBL4793852 | — | — | 1 | 7.68 |
| CHEMBL4776057 | — | — | 1 | 7.62 |
| CHEMBL4755832 | — | — | 1 | 7.57 |
| CHEMBL4749765 | — | — | 1 | 7.55 |
| CHEMBL4741678 | — | — | 1 | 7.54 |
| CHEMBL4760864 | — | — | 1 | 7.52 |
| CHEMBL4747893 | — | — | 1 | 7.41 |
| CHEMBL4750608 | — | — | 1 | 7.37 |
| CHEMBL4790583 | — | — | 1 | 7.36 |
| CHEMBL4796407 | — | — | 1 | 7.30 |
| CHEMBL4759414 | — | — | 1 | 7.29 |
| CHEMBL4763967 | — | — | 1 | 7.28 |
| CHEMBL4760606 | — | — | 1 | 7.24 |
| CHEMBL4743173 | — | — | 1 | 7.17 |
| CHEMBL4757531 | — | — | 1 | 6.77 |
| CHEMBL4777554 | — | — | 1 | 6.76 |
| CHEMBL4751768 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4789811 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4792426 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4790655 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4752951 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4750196 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4777353 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4757724 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4782025 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4745521 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4754811 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4753193 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4743566 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4793852 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4776057 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4755832 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4749765 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4741678 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4760864 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4747893 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4750608 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4790583 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4796407 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4759414 | — | IC50 | = | 50.9 | nM | 7.29 |
| CHEMBL4763967 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4760606 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4743173 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4757531 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL4777554 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4751768 | — | IC50 | = | 242.4 | nM | 6.62 |
| CHEMBL4762998 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL4755444 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL4756049 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4790485 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL4763697 | — | IC50 | = | 722.0 | nM | 6.14 |
| CHEMBL4784185 | — | IC50 | = | 2426.0 | nM | 5.62 |